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In conclusion we show that HBP is phosphorylated on three
2024-06-19
In conclusion, we show that HBP1 is phosphorylated on three sites, which control HBP1 transcriptional activity and glioblastoma cell proliferation. This phosphorylation largely depends on AKT, although other kinases may also be involved. In a previous study, we had shown that the PI3K-AKT pathway re
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Cancers that responded to immune checkpoint inhibitors were
2024-06-19
Cancers that responded to immune checkpoint inhibitors were shown to present a type I interferon (IFN) signature in the TME 33, 34. Type I IFNs positively regulate the expression of tumor antigens and their crosspresentation by DCs to tumoricidal CTLs. Furthermore, CD8+ T cell develops full effector
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Derivatives of M that possess either an alkyne or
2024-06-19
Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these ACY-241 to maintain 5-HTR antagonist properties as (+)-M100907 was demonstrated
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Previous studies have demonstrated the presence of soluble N
2024-06-19
Previous studies have demonstrated the presence of soluble NTPDases, 5′-nucleotidase and adenosine deaminase in rat blood serum as well as in human blood (Doleski et al., 2016; Oses et al., 2004; Yegutkin, 1997; Yegutkin et al., 2007). In addition, our earlier reports have shown that these membrane-
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br There is evidence to suggest that
2024-06-19
There is evidence to suggest that GMF activities are regulated in vivo by post-translational modification. indeed, there is strong precedent for ADF-homology family proteins being regulated in this manner. Cofilin is inhibited by phosphorylation of a serine residue at its N terminus. This residue
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Previously we described that cadmium induces a more
2024-06-19
Previously, we described that cadmium induces a more pronounced, but not selective, cell death on primary cholinergic neurons from basal forebrain (Del Pino et al., 2014). Degeneration of septal cholinergic neurons from basal forebrain, as happens in AD, results in memory deficits (Scheiderer et al.
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It has been reported that
2024-06-19
It has been reported that 5-HT2R involves in type 2 diabetes mellitus and 5-HT-induced IR [22,23]. The present study also demonstrated that it is 5-HT2R rather than other 5-HT receptors, including 5-HT1BR and 5-HT7R, in the liver that mediates HFD-induced abnormality of hepatic lipid metabolism, and
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The ATX LPA signaling axis has been implicated in a
2024-06-18
The ATX–LPA signaling “axis” [5] has been implicated in a perplexing variety of physiological and pathophysiological processes, including vascular and neural development [5], [26], [27], [28], [29], tumor progression and metastasis [30], [31], lymphocyte trafficking [22], bone development [32], neur
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br Acknowledgements Authors wish to thank Sabanci University
2024-06-18
Acknowledgements Authors wish to thank Sabanci University (Turkey), Tubitak (Cost Eu-Ros, 113Z463), and the University of Turin (Italy) for supporting this work. Beyza Vurusaner is supported by Sabanci University Post-doctoral research scholarship. Introduction Endometriosis is defined as the
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Another important question concerns the
2024-06-18
Another important question concerns the mechanism by which a polyubiquitinated substrate is released from the Cdc48 complex and passed on to downstream components, such as the proteasome. There are at least three proposed models. In the first, a ubiquitinated substrate is transferred by ubiquitin-bi
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br Future directions outlook Peptide based macrocycles are a
2024-06-18
Future directions-outlook Peptide-based macrocycles are among the privileged scaffolds in antibiotic drug discovery. Many compounds were discovered by natural product screening and developed unchanged, or as semi-synthetic derivatizations. Since the golden age of antibiotic discovery (1940s-mid 1
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br Nanoparticle Conjugated Topoisomerase Inhibitors The safe
2024-06-18
Nanoparticle-Conjugated Topoisomerase Inhibitors The safety and efficacy of topotecan administered as LDM or MTD have been evaluated in several preclinical studies and a few clinical trials whose results showed that there can be significant adverse effects likely precluding its use in patients [5
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Tumor tissues often experience hypoxia owing to
2024-06-18
Tumor tissues often experience hypoxia owing to accelerated growth rates of malignant cells, accumulation of metabolic products, disorganization of tumor blood vessels, and high interstitial fluid pressures (Makino et al., 2001). In response to AAD treatment, tumor vascular density often decreases t
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We recently identified a G A dependent epigenetic
2024-06-18
We recently identified a G9A-dependent epigenetic mechanism for transcriptional activation of the serine pathway in cancer cells (Ding et al., 2013). G9A, also known as EHMT2 and KMT1C, is a H3K9 methyltransferase that has a primary role in catalyzing H3K9me1 and H3K9me2 in euchromatin (Shinkai and
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Gratifyingly compound also demonstrated improved physicochem
2024-06-18
Gratifyingly, compound also demonstrated improved physicochemical properties with significant improvement in aqueous solubility. Compound was sufficiently potent to determine its pharmacokinetic (PK) and pharmacodynamics (PD); data is summarized in . shows ADME characteristics for compound and
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